EP1423111A4 - Composes de liaison au recepteur nucleaire fxr nr1h4 - Google Patents

Composes de liaison au recepteur nucleaire fxr nr1h4

Info

Publication number: EP1423111A4
Authority: EP; European Patent Office
Prior art keywords: fxr; nuclear receptor; receptor binding; binding compounds; nr1h4
Prior art date: 2001-08-13
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.): Withdrawn

Application number

EP02750473A

Other languages

German (de)

English (en)

Other versions

EP1423111A1 (fr

Inventor

Ulrike Bauer

Zach Cheruvallath

Ulrich Deuschle

Elena Dneprovskaia

Tim Gahman

Kristina Giegrich

Ronnie Hanecak

Normand Hebert

John Kiely

Ingo Kober

Manfred Kogl

Harald Kranz

Claus Kremoser

Matthew Lee

Kerstin Otte

Carlton Sage

Manish Sud

Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)

Phenex Pharmaceuticals AG

Original Assignee

Phenex Pharmaceuticals AG

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

2001-08-13

Filing date

2002-08-13

Publication date

2007-04-18

2002-08-13 Application filed by Phenex Pharmaceuticals AG filed Critical Phenex Pharmaceuticals AG

2002-08-13 Priority to EP02750473A priority Critical patent/EP1423111A4/fr

2004-06-02 Publication of EP1423111A1 publication Critical patent/EP1423111A1/fr

2007-04-18 Publication of EP1423111A4 publication Critical patent/EP1423111A4/fr

Status Withdrawn legal-status Critical Current

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
- C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
- C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
- C07D261/08—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
- C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/11—Compounds covalently bound to a solid support

Landscapes

Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Health & Medical Sciences (AREA)
Animal Behavior & Ethology (AREA)
General Health & Medical Sciences (AREA)
Veterinary Medicine (AREA)
Public Health (AREA)
Life Sciences & Earth Sciences (AREA)
Pharmacology & Pharmacy (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Medicinal Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Obesity (AREA)
Hematology (AREA)
Child & Adolescent Psychology (AREA)
Diabetes (AREA)
Cardiology (AREA)
Heart & Thoracic Surgery (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

EP02750473A 2001-08-13 2002-08-13 Composes de liaison au recepteur nucleaire fxr nr1h4 Withdrawn EP1423111A4 (fr)

Priority Applications (1)

Application Number	Priority Date	Filing Date	Title
EP02750473A EP1423111A4 (fr)	2001-08-13	2002-08-13	Composes de liaison au recepteur nucleaire fxr nr1h4

Applications Claiming Priority (6)

Application Number	Priority Date	Filing Date	Title
US185721		1980-09-19
EP01119473		2001-08-13
EP01119473A EP1285914B1 (fr)	2001-08-13	2001-08-13	Ligands du récepteur nucéaire nr1h4
US10/185,721 US7034046B2 (en)	2001-08-13	2002-07-01	NR1H4 nuclear receptor binding compounds
PCT/US2002/025437 WO2003015771A1 (fr)	2001-08-13	2002-08-13	Composes de liaison au recepteur nucleaire fxr nr1h4
EP02750473A EP1423111A4 (fr)	2001-08-13	2002-08-13	Composes de liaison au recepteur nucleaire fxr nr1h4

Publications (2)

Publication Number	Publication Date
EP1423111A1 EP1423111A1 (fr)	2004-06-02
EP1423111A4 true EP1423111A4 (fr)	2007-04-18

Family

ID=8178316

Family Applications (3)

Application Number	Title	Priority Date	Filing Date
EP01119473A Expired - Lifetime EP1285914B1 (fr)	2001-08-13	2001-08-13	Ligands du récepteur nucéaire nr1h4
EP02750472A Withdrawn EP1423370A4 (fr)	2001-08-13	2002-08-13	Composes de liaison au recepteur nucleaire fxr nr1h4
EP02750473A Withdrawn EP1423111A4 (fr)	2001-08-13	2002-08-13	Composes de liaison au recepteur nucleaire fxr nr1h4

Family Applications Before (2)

Application Number	Title	Priority Date	Filing Date
EP01119473A Expired - Lifetime EP1285914B1 (fr)	2001-08-13	2001-08-13	Ligands du récepteur nucéaire nr1h4
EP02750472A Withdrawn EP1423370A4 (fr)	2001-08-13	2002-08-13	Composes de liaison au recepteur nucleaire fxr nr1h4

Country Status (5)

Country	Link
US (3)	US6974830B2 (fr)
EP (3)	EP1285914B1 (fr)
AT (1)	ATE381542T1 (fr)
DE (1)	DE60131967D1 (fr)
WO (2)	WO2003015771A1 (fr)

Families Citing this family (97)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US7138390B2 (en)	2001-03-12	2006-11-21	Intercept Pharmaceuticals	Steroids as agonists for FXR
US6987121B2 (en) *	2002-04-25	2006-01-17	Smithkline Beecham Corporation	Compositions and methods for hepatoprotection and treatment of cholestasis
US20060148858A1 (en) *	2002-05-24	2006-07-06	Tsuyoshi Maekawa	1, 2-Azole derivatives with hypoglycemic and hypolipidemic activity
US7319109B2 (en)	2002-11-22	2008-01-15	Smith Kline Beecham Corporation	Farnesoid X receptor agonists
BRPI0414812A (pt) *	2003-09-26	2006-11-14	Forbes Medi Tech Inc	método de inibir a expressão de genes resistentes a múltiplos medicamentos e de inibir a produção de proteìnas resultantes da expressão de tais gene, melhorando assim a efetividade dos agentes quimioterápicos para tratar cánceres
WO2005042692A2 (fr) *	2003-10-31	2005-05-12	Forbes Medi-Tech Inc.	Methode permettant d'inhiber l'expression de genes qui induisent l'influx de cholesterol cellulaire dans les cellules animales et d'inhiber la production de proteines issues de l'expression de ces genes
CA2546601A1 (fr)	2003-11-19	2005-06-09	Metabasis Therapeutics, Inc.	Nouvelles substances thyromimetiques contenant du phosphore
PL1700856T3 (pl) *	2003-12-26	2016-05-31	Kyowa Hakko Kirin Co Ltd	Pochodna tiazolu
PT1734970E (pt)	2004-03-12	2015-03-11	Intercept Pharmaceuticals Inc	Tratamento de fibrose utilizando ligandos de rfx
US10987362B2 (en)	2004-03-12	2021-04-27	Intercept Pharmaceuticals, Inc.	Treatment of fibrosis using FXR ligands
US20060019907A1 (en) *	2004-07-12	2006-01-26	Research Development Foundation	Guggulsterone: an inhibitor of nuclear factor - kappaB and IkappaBalpha kinase activation and uses thereof
WO2006012642A2 (fr)	2004-07-30	2006-02-02	Exelixis, Inc.	Derives de pyrrole en tant qu'agents pharmaceutiques
WO2006029719A2 (fr) *	2004-09-14	2006-03-23	Bayer Healthcare Ag	Diagnostics et traitements de maladies associees a la sous-famille 1, du groupe h, membre 4 de recepteur nucleaire (nr1h4)
US20060252670A1 (en) *	2004-10-14	2006-11-09	Intercept Pharmaceuticals Inc.	Method of reducing drug-induced adverse side effects in a patient
ITMI20050912A1 (it) *	2005-05-19	2006-11-20	Erregierre Spa	Processo di preparazione di acidi 3-a-ya(b)-diidrossi-6-a(b)-alchil-5b-colanici
US20090232879A1 (en)	2005-05-26	2009-09-17	Metabasis Therapeutics, Inc.	Thyromimetics for the Treatment of Fatty Liver Diseases
US7618956B2 (en) *	2005-05-31	2009-11-17	The Gillette Company	Reduction of hair growth
WO2007052843A1 (fr) *	2005-11-04	2007-05-10	Takeda Pharmaceutical Company Limited	Compose amide heterocyclique et son utilisation
US7705028B2 (en)	2005-12-19	2010-04-27	Glaxosmithkline Llc	Farnesoid X receptor agonists
CN101374834B (zh) *	2006-02-03	2011-12-14	伊莱利利公司	用于调节fxr的化合物和方法
PE20080259A1 (es) *	2006-05-24	2008-04-10	Lilly Co Eli	Compuestos y metodos para modular fxr
US7846960B2 (en)	2006-05-24	2010-12-07	Eli Lilly And Company	FXR agonists
EP1886685A1 (fr) *	2006-08-11	2008-02-13	INSERM (Institut National de la Santé et de la Recherche Médicale)	Méthodes, utilisations et compositions pour la modulation de la réplication du HCV par activation ou inhibition du récepteur farnesoid X
EP1894928A1 (fr) *	2006-08-29	2008-03-05	PheneX Pharmaceuticals AG	Composes heterocycliques de liaison au fxr
EP1894924A1 (fr) *	2006-08-29	2008-03-05	Phenex Pharmaceuticals AG	Composés hétérocycliques de liason du FXR
CL2007003035A1 (es) *	2006-10-24	2008-05-16	Smithkline Beechman Corp	Compuestos derivados de isoxazol sustituidos, agonistas de receptores farnesoid x; procedimiento de preparacion; composicion farmaceutica que lo comprende; y uso del compuesto en el tratamiento de la obesidad, diabetes mellitus, fibrosis en organos,
CA2928178C (fr)	2007-01-19	2019-09-10	Intercept Pharmaceuticals, Inc.	Modulateurs de tgr5 et leurs procedes d'utilisation
EP2173174A4 (fr) *	2007-07-02	2010-08-04	Glaxosmithkline Llc	Agonistes du récepteur de farnésoïde x
TW200906823A (en)	2007-07-16	2009-02-16	Lilly Co Eli	Compounds and methods for modulating FXR
US7902201B2 (en)	2007-12-04	2011-03-08	Hoffmann-La Roche Inc.	Isoxazolo-pyrazine derivatives
US7943619B2 (en)	2007-12-04	2011-05-17	Hoffmann-La Roche Inc.	Isoxazolo-pyridazine derivatives
BRPI0820649A2 (pt)	2007-12-04	2015-06-16	Hoffmann La Roche	Derivados de isoxazalo-pirazina
EP2128158A1 (fr)	2008-05-26	2009-12-02	Phenex Pharmaceuticals AG	Composés de liaison FXR substitués de cyclopropyle hétérocyclique
EA020310B1 (ru)	2008-07-30	2014-10-30	Интерсепт Фармасьютикалз, Инк.	Модуляторы рецептора tgr5 и их применение
UA107917C2 (ru) *	2008-10-21	2015-03-10	Сімабей Терапьютікс, Інк.	Арильный агонист рецептора gpr120 и его применение
AU2009316566B9 (en)	2008-11-19	2014-05-15	Intercept Pharmaceuticals, Inc.	TGR5 modulators and method of use thereof
US20110257139A1 (en)	2008-12-19	2011-10-20	Royal College Of Surgeons In Ireland	Treatment of diarrhoea
TW201033201A (en)	2009-02-19	2010-09-16	Hoffmann La Roche	Isoxazole-isoxazole and isoxazole-isothiazole derivatives
US8389550B2 (en)	2009-02-25	2013-03-05	Hoffmann-La Roche Inc.	Isoxazoles / O-pyridines with ethyl and ethenyl linker
US8222246B2 (en)	2009-04-02	2012-07-17	Hoffmann-La Roche Inc.	Substituted isoxazoles
US8227461B2 (en)	2009-04-30	2012-07-24	Hoffmann-La Roche Inc.	Isoxazoles
US8410104B2 (en)	2009-05-05	2013-04-02	Hoffmann-La Roche Inc.	Pyridazines
JP5466292B2 (ja)	2009-05-05	2014-04-09	エフ．ホフマン−ラロシュアーゲー	イソオキサゾール−ピリジン誘導体
CN102414208B (zh)	2009-05-05	2014-11-05	霍夫曼-拉罗奇有限公司	作为用于认知性障碍的治疗中的gaba a受体逆激动剂的异*唑-噻唑衍生物
CA2760746C (fr)	2009-05-05	2017-07-11	F. Hoffmann-La Roche Ag	Derives d'isoxazole-pyrazole
BRPI1013766A2 (pt)	2009-05-07	2016-04-05	Hoffmann La Roche	"derivados de isoxazol-piridina como moduladores de gaba"
EP2289883A1 (fr) *	2009-08-19	2011-03-02	Phenex Pharmaceuticals AG	Nouveaux composés modulant l'activité du recepteur FXR (NR1H4)
EP2545964A1 (fr)	2011-07-13	2013-01-16	Phenex Pharmaceuticals AG	Nouveaux composés se liant au fxr (nr1 h4) et modulant son activité
WO2013037482A1 (fr)	2011-09-15	2013-03-21	Phenex Pharmaceuticals Ag	Agonistes du récepteur du farnésoïde x pour le traitement et la prévention du cancer
US8785435B2 (en)	2011-10-20	2014-07-22	Hoffmann-La Roche Inc.	Solid forms
ES2822375T3 (es)	2012-06-19	2021-04-30	Intercept Pharmaceuticals Inc	Preparación de la forma no cristalina del ácido obeticólico
US9982008B2 (en)	2012-06-19	2018-05-29	Intercept Pharmaceuticals, Inc.	Preparation and uses of obeticholic acid
LT3043865T (lt)	2013-09-11	2021-04-26	Institut National De La Santé Et De La Recherche Médicale (Inserm)	Hepatito b viruso infekcijos gydymo būdai ir farmacinė kompozicija
EP3006939A1 (fr)	2014-10-06	2016-04-13	Gilead Sciences, Inc.	Glycoprotéine riche en histidine comme marqueur de l'activation du récepteur farnésoïde X hépatique
US10208081B2 (en)	2014-11-26	2019-02-19	Enanta Pharmaceuticals, Inc.	Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof
EP3034501A1 (fr)	2014-12-17	2016-06-22	Gilead Sciences, Inc.	Hydroxy contenant des composés de modulation (FXR NR1H4)
EP3034499A1 (fr)	2014-12-17	2016-06-22	Gilead Sciences, Inc.	Nouveaux composés de modulation (FXR NR1H4)
ES2905872T3 (es)	2015-02-06	2022-04-12	Intercept Pharmaceuticals Inc	Composiciones farmacéuticas para terapia combinada
TWI698430B (zh)	2015-02-13	2020-07-11	南北兄弟藥業投資有限公司	三環化合物及其在藥物中的應用
NZ735126A (en)	2015-03-31	2022-10-28	Enanta Pharm Inc	Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof
CN107613986A (zh)	2015-04-07	2018-01-19	英特塞普特医药品公司	用于组合疗法的药物组合物
WO2017189663A1 (fr)	2016-04-26	2017-11-02	Enanta Pharmaceuticals, Inc.	Dérivés d'isoxazole utilisés comme agonistes de fxr et leurs méthodes d'utilisation
WO2017189652A1 (fr)	2016-04-26	2017-11-02	Enanta Pharmaceuticals, Inc.	Dérivés d'isoxazole utilisés comme agonistes de fxr et leurs procédés d'utilisation
US10080742B2 (en)	2016-04-26	2018-09-25	Enanta Pharmaceuticals, Inc.	Isoxazole derivatives as FXR agonists and methods of use thereof
WO2017201152A1 (fr)	2016-05-18	2017-11-23	Enanta Pharmaceuticals, Inc.	Dérivés d'isoxazole utilisés comme agonistes de fxr et leurs procédés d'utilisation
US10149835B2 (en)	2016-05-18	2018-12-11	Elmore Patent Law Group, P.C.	Isoxazole derivatives as FXR agonists and methods of use thereof
WO2017201150A1 (fr)	2016-05-18	2017-11-23	Enanta Pharmaceuticals, Inc.	Analogues de l'isoxazole comme agonistes de fxr et leurs procédés d'utilisation
CA3252823A1 (en)	2016-06-13	2025-02-25	Gilead Sciences Inc	Fxr (nr1h4) modulating compounds
SI3730487T1 (sl)	2016-06-13	2022-08-31	Gilead Sciences, Inc.	Azetidinski derivati kot modulatorji FXR (NR1H4)
TW201808283A (zh)	2016-08-05	2018-03-16	廣東東陽光藥業有限公司	含氮三環化合物及其在藥物中的應用
CA3039124A1 (fr)	2016-10-04	2018-04-12	Enanta Pharmaceuticals, Inc.	Analogues de l'isoxazole en tant qu'agonistes de fxr et leurs procedes d'utilisation
US10597391B2 (en)	2016-10-26	2020-03-24	Enanta Pharmaceuticals, Inc.	Urea-containing isoxazole derivatives as FXR agonists and methods of use thereof
JP2020500199A (ja)	2016-11-21	2020-01-09	バイキング・セラピューティクス・インコーポレイテッド	グリコーゲン蓄積症の治療方法
JP6906626B2 (ja)	2017-03-28	2021-07-21	ギリアードサイエンシーズ，インコーポレイテッド	肝疾患を処置するための治療的組み合わせ
EP3600293A1 (fr)	2017-03-30	2020-02-05	Institut National de la Sante et de la Recherche Medicale (INSERM)	Méthodes et compositions pharmaceutiques pour réduire la persistance et l'expression des virus épisomiques
RS62711B1 (sr)	2017-04-12	2022-01-31	Il Dong Pharma	Derivati izoksazola kao agonisti nuklearnih receptora i njihova upotreba
AU2018280118B2 (en)	2017-06-05	2021-07-15	Viking Therapeutics, Inc.	Compositions for the treatment of fibrosis
CN111630051B (zh)	2017-11-01	2023-12-26	百时美施贵宝公司	作为法尼醇x受体调节剂的烯烃螺环化合物
KR102732404B1 (ko)	2017-11-01	2024-11-19	브리스톨-마이어스 스큅 컴퍼니	파르네소이드 x 수용체 조정제로서의 알켄 화합물
US11370785B2 (en)	2017-11-01	2022-06-28	Bristol-Myers Squibb Company	Multicyclic compounds as farnesoid X receptor modulators
WO2019118571A1 (fr)	2017-12-12	2019-06-20	Enanta Pharmaceuticals, Inc.	Analogues de l'isoxazole utilisés en tant qu'agonistes de fxr et leurs procédés d'utilisation
CN110128432B (zh)	2018-02-02	2021-03-02	广东东阳光药业有限公司	含氮三环化合物及其在药物中的应用
US10829486B2 (en)	2018-02-14	2020-11-10	Enanta Pharmacueticals, Inc.	Isoxazole derivatives as FXR agonists and methods of use thereof
EA202091979A1 (ru)	2018-03-22	2021-06-22	Вайкинг Терапьютикс, Инк.	Кристаллические формы и способы получения кристаллических форм соединения
IT201800007265A1 (it) *	2018-07-17	2020-01-17		Isossazoli come agonisti del recettore fxr
US12102646B2 (en)	2018-12-05	2024-10-01	Viking Therapeutics, Inc.	Compositions for the treatment of fibrosis and inflammation
US11225473B2 (en)	2019-01-15	2022-01-18	Gilead Sciences, Inc.	FXR (NR1H4) modulating compounds
EP3927683A1 (fr)	2019-02-19	2021-12-29	Gilead Sciences, Inc.	Formes solides d'agonistes de fxr
US11555032B2 (en)	2019-05-13	2023-01-17	Enanta Pharmaceuticals, Inc.	Isoxazole derivatives as FXR agonists and methods of use thereof
WO2020243590A1 (fr)	2019-05-30	2020-12-03	Intercept Pharmaceuticals, Inc.	Compositions pharmaceutiques comprenant un agoniste de fxr et un fibrate pour une utilisation dans le traitement d'une maladie hépatique cholestatique
WO2021009332A1 (fr)	2019-07-18	2021-01-21	Enyo Pharma	Procédé pour diminuer les effets secondaires de l'interféron
CN112824394B (zh) *	2019-11-21	2024-08-13	中国科学院上海药物研究所	PPARs-FXR多靶点小分子激动剂及其制备方法和用途
WO2021108974A1 (fr) *	2019-12-03	2021-06-10	Gannex Pharma Co., Ltd	Composés pour moduler l'activité du fxr et leurs utilisations
CA3159163A1 (fr)	2020-01-15	2021-07-22	Raphael Darteil	Utilisation d'agonistes de fxr pour traiter une infection par le virus de l'hepatite d
US11478533B2 (en)	2020-04-27	2022-10-25	Novo Nordisk A/S	Semaglutide for use in medicine
CA3204800A1 (fr)	2021-01-14	2022-07-21	Raphael Darteil	Effet synergique d'un agoniste de fxr et d'ifn pour le traitement d'une infection par le virus de l'hepatite b
US20240216364A1 (en)	2021-04-28	2024-07-04	Enyo Pharma	Strong potentiation of tlr3 agonists effects using fxr agonists as a combined treatment

Citations (1)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
DE3621372A1 (de) *	1986-06-26	1988-01-07	Thomae Gmbh Dr K	Heterocyclisch substituierte 3,5-dihydroxy-hept-6-en-carbonsaeuren, ihre derivate, verfahren zur herstellung dieser verbindungen und die sie enthaltende arzneimittel

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US2863874A (en) *	1955-05-26	1958-12-09	Goodrich Co B F	Process of preparing 2-aminothiazoles
AU545463B2 (en) *	1982-06-25	1985-07-18	Kowa Co. Ltd.	Benzoyl piperacine esters
JPS59139357A (ja) *	1983-01-28	1984-08-10	Torii Yakuhin Kk	アミジン誘導体
DE4237768A1 (en) *	1991-11-12	1993-05-13	Ciba Geigy Ag	New polyarylene ether derivs. with reduced viscosity - used to prepare moulded bodies, foils, fibres and membranes, as matrix resins, adhesives or coating agents or as polymer additives
DE4219247A1 (de) *	1992-06-12	1993-12-16	Bayer Ag	Verwendung von 3-arylsubstituierten 5-Alkyl-isoxazol-4-carbonsäurederivaten zur Bekämpfung von Endoparasiten, neue 3-arylsubstituierte 5-Alkyl-isoxazol-4-carbonsäurederivate und Verfahren zu ihrer Herstellung
FR2692893B1 (fr) *	1992-06-24	1994-09-02	Sanofi Elf	Dérivés alkylamino ramifiés du thiazole, leurs procédés de préparation et les compositions pharmaceutiques qui les contiennent.
US6005103A (en) *	1993-11-19	1999-12-21	Warner-Lambert Company	Pyrone derivatives as protease inhibitors and antiviral agents
FR2714059B1 (fr) *	1993-12-21	1996-03-08	Sanofi Elf	Dérivés amino ramifiés du thiazole, leurs procédés de préparation et les compositions pharmaceutiques qui les contiennent.
AU3201095A (en) *	1994-07-27	1996-02-22	G.D. Searle & Co.	Substituted thiazoles for the treatment of inflammation
KR980700077A (ko) *	1994-11-29	1998-03-30	나까토미 히로타카	2-아미노티아졸유도체 및 그 염류로 이루어진 항균제 또는 살균제(Antibacterial Prepartion or Bactericide comprising 2-Aminothiazole Derivative or Salt Thereof
PL185544B1 (pl) *	1995-02-13	2003-05-30		Nowa pochodna podstawionego izoksazolu i środek farmaceutyczny
CA2190973C (fr) *	1995-04-13	2001-06-19	Yasuo Konno	Nouveaux derives 4,6-diarylpyrimidine et leurs sels
JP4136024B2 (ja)	1995-12-29	2008-08-20	富山化学工業株式会社	２−アミノチアゾ−ル誘導体またはその塩
US5883105A (en)	1996-04-03	1999-03-16	Merck & Co., Inc.	Inhibitors of farnesyl-protein transferase
JPH11263775A (ja) *	1997-09-08	1999-09-28	Sankyo Co Ltd	ヒドロキシアニリン誘導体
US6262098B1 (en) *	1998-08-07	2001-07-17	Chiron Corporation	Estrogen receptor modulators
EP1140079B1 (fr) *	1998-12-23	2009-06-03	Glaxo Group Limited	Methodes de titrage de ligands de recepteurs nucleaires
US6201020B1 (en) *	1998-12-31	2001-03-13	Guilford Pharmaceuticals, Inc.	Ortho-diphenol compounds, methods and pharmaceutical compositions for inhibiting parp
EE200100558A (et) *	1999-04-28	2002-12-16	Aventis Pharma Deutschland Gmbh	Triarüülhappe derivaat, seda sisaldav farmatseutiline kompositsioon ja ühendi raviotstarbeline kasutamine
DE19943636A1 (de) *	1999-09-13	2001-03-15	Bayer Ag	Neuartige Dicarbonsäurederivate mit pharmazeutischen Eigenschaften
JP5074653B2 (ja) *	2000-03-29	2012-11-14	サイクラセルリミテッド	２−置換４−ヘテロアリール−ピリミジンおよび増殖性障害におけるその使用
GB0030710D0 (en) *	2000-12-15	2001-01-31	Hoffmann La Roche	Piperazine derivatives

2001
- 2001-08-13 DE DE60131967T patent/DE60131967D1/de not_active Expired - Lifetime
- 2001-08-13 AT AT01119473T patent/ATE381542T1/de not_active IP Right Cessation
- 2001-08-13 EP EP01119473A patent/EP1285914B1/fr not_active Expired - Lifetime
2002
- 2002-07-01 US US10/185,731 patent/US6974830B2/en not_active Expired - Lifetime
- 2002-07-01 US US10/185,721 patent/US7034046B2/en not_active Expired - Lifetime
- 2002-08-13 EP EP02750472A patent/EP1423370A4/fr not_active Withdrawn
- 2002-08-13 WO PCT/US2002/025437 patent/WO2003015771A1/fr not_active Ceased
- 2002-08-13 WO PCT/US2002/025436 patent/WO2003016288A1/fr not_active Ceased
- 2002-08-13 EP EP02750473A patent/EP1423111A4/fr not_active Withdrawn
- 2002-08-13 US US10/217,141 patent/US7098336B2/en not_active Expired - Fee Related

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
DE3621372A1 (de) *	1986-06-26	1988-01-07	Thomae Gmbh Dr K	Heterocyclisch substituierte 3,5-dihydroxy-hept-6-en-carbonsaeuren, ihre derivate, verfahren zur herstellung dieser verbindungen und die sie enthaltende arzneimittel

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
A.E. HYDORN ET AL, J. ORG. CHEM, vol. 27, 1962, pages 4305 - 4309, XP002421611 *
LIM JUNG KI ET AL: "Analgesic, anti-inflammatory and antiviral effects of melandrin derivatives", CAPLUS, 1994, XP002958754 *
P.R. MALONEY ET AL, J. MED. CHEM., vol. 43, no. 16, 2000, pages 2971 - 2974, XP002421612 *

Also Published As

Publication number	Publication date
EP1423111A1 (fr)	2004-06-02
US20030187042A1 (en)	2003-10-02
EP1423370A1 (fr)	2004-06-02
ATE381542T1 (de)	2008-01-15
WO2003016288A1 (fr)	2003-02-27
EP1285914A1 (fr)	2003-02-26
US20030130296A1 (en)	2003-07-10
DE60131967D1 (de)	2008-01-31
WO2003015771A1 (fr)	2003-02-27
US7098336B2 (en)	2006-08-29
US6974830B2 (en)	2005-12-13
EP1285914B1 (fr)	2007-12-19
EP1423370A4 (fr)	2007-04-18
US20030149087A1 (en)	2003-08-07
US7034046B2 (en)	2006-04-25

Publication	Publication Date	Title
EP1423370A4 (fr)	2007-04-18	Composes de liaison au recepteur nucleaire fxr nr1h4
MXPA03011484A (es)	2004-03-18	Heteroarilos multiciclicos sustituidos con quinuclidinas para el tratamiento de enfermedades.
WO2003028641A3 (fr)	2003-08-28	Antagonistes du recepteur de la mch
DE60231341D1 (de)	2009-04-09	Fluor- und sulfonylaminohaltige, 3,6-disubstituierptorantagonisten
PL1716152T3 (pl)	2009-01-30	Skondensowane związki heterocykliczne i ich zastosowanie jako antagonistów receptora metabotropowego do leczenia zaburzeń żołądkowo-jelitowych
BG108650A (en)	2005-04-30	Azabicyclic-substituted fused-heteroaryl compounds for the treatment of disease
EA200601266A1 (ru)	2007-02-27	Соединения триазола и их применение в качестве антагонистов метаботропного рецептора глутамата
ATE396186T1 (de)	2008-06-15	Heteroarylsubstituierte tetrazolmodulatoren des metabotropischen glutamatrezeptors-5
WO2002060900A8 (fr)	2003-11-06	Antagonistes vis-a-vis de la fonction mcp-1 et procedes d'utilisation
MXPA04004464A (es)	2004-08-11	Compuestos de heteroarilo sustituido con azabiciclo para el tratamiento de enfermedades.
WO2004091514A3 (fr)	2005-09-15	Antagonistes des recepteurs de cgrp
BR0314688A (pt)	2005-08-02	Novos derivados de piperidina para utilização no tratamento de estados de doença mediados pela quimiocina
DE60237528D1 (de)	2010-10-14	Neue aminoazetidin-, aminopyrrolidin- und aminopiperidinderivative
EP1398029A8 (fr)	2004-06-16	Derivés de pyrazole,substitués en position 3 ayant une affinité envers le NR3B1 récepteur
NO20063275L (no)	2006-07-14	Anvendelse av substituerte 2-aminotetraliner for forebyggende behandling av Parkinsons sykdom
TW200502221A (en)	2005-01-16	Novel lactams and uses thereof
ATE342253T1 (de)	2006-11-15	Azabicycloderivate als antagonisten des muscarinischen rezeptors
ATE377602T1 (de)	2007-11-15	Morphinanderivate und ihre medizinische anwendung
TW200621753A (en)	2006-07-01	Pyrimidinylimidazoles and methods of making and using the same
DE60226906D1 (de)	2008-07-10	3,6-disubstituierte azabicyclo ä3.1.0ühexanderivate, die sich als muscarinrezeptorantagonisten eignen
TW200720260A (en)	2007-06-01	Prokineticin 1 receptor antagonists
WO2007079163A3 (fr)	2007-08-30	Antagonistes du recepteur de la prokineticine 1
NZ543632A (en)	2009-02-28	Benzimidazole derivatives, compositions containing them, preparation thereof and uses thereof
ATE370147T1 (de)	2007-09-15	Thiazolopyrimidinderivate und deren verwendung als antagonisten des cx3cr1 rezeptors
EA200501594A1 (ru)	2006-08-25	Замещенные производные азабициклогексана в качестве антагонистов мускаринового рецептора

Legal Events

Date	Code	Title	Description
2004-04-16	PUAI	Public reference made under article 153(3) epc to a published international application that has entered the european phase	Free format text: ORIGINAL CODE: 0009012
2004-06-02	17P	Request for examination filed	Effective date: 20040225
2004-06-02	AK	Designated contracting states	Kind code of ref document: A1 Designated state(s): AT BE BG CH CY CZ DE DK EE ES FI FR GB GR IE IT LI LU MC NL PT SE SK TR
2004-06-02	AX	Request for extension of the european patent	Extension state: AL LT LV MK RO SI
2004-06-16	RIN1	Information on inventor provided before grant (corrected)	Inventor name: SUD, MANISH Inventor name: SAGE, CARLTON Inventor name: OTTE, KERSTIN Inventor name: LEE, MATTHEW Inventor name: KREMOSER, CLAUS Inventor name: KRANZ, HARALD Inventor name: KOGL, MANFRED Inventor name: KOBER, INGO Inventor name: KIELY, JOHN Inventor name: HEBERT, NORMAND Inventor name: HANECAK, RONNIE Inventor name: GIEGRICH, KRISTINA Inventor name: GAHMAN, TIM Inventor name: DNEPROVSKAIA, ELENA Inventor name: DEUSCHLE, ULRICH Inventor name: CHERUVALLATH, ZACH Inventor name: BAUER, ULRIKE
2004-06-30	RIN1	Information on inventor provided before grant (corrected)	Inventor name: SUD, MANISH Inventor name: SAGE, CARLTON Inventor name: OTTE, KERSTIN Inventor name: LEE, MATTHEW Inventor name: KREMOSER, CLAUS Inventor name: KRANZ, HARALD Inventor name: KOGL, MANFRED Inventor name: KOBER, INGO Inventor name: KIELY, JOHN Inventor name: HEBERT, NORMAND Inventor name: HANECAK, RONNIE Inventor name: GIEGRICH, KRISTINA Inventor name: GAHMAN, TIM Inventor name: DNEPROVSKAIA, ELENA Inventor name: DEUSCHLE, ULRICH Inventor name: CHERUVALLATH, ZACH Inventor name: BAUER, ULRIKE
2004-12-01	RAP1	Party data changed (applicant data changed or rights of an application transferred)	Owner name: PHENEX PHARMACEUTICALS AG
2006-04-05	RAP1	Party data changed (applicant data changed or rights of an application transferred)	Owner name: PHENEX PHARMACEUTICALS AG
2007-04-18	A4	Supplementary search report drawn up and despatched	Effective date: 20070319
2008-06-18	17Q	First examination report despatched	Effective date: 20080516
2008-11-05	RIN1	Information on inventor provided before grant (corrected)	Inventor name: SUD, MANISH Inventor name: SAGE, CARLTON Inventor name: OTTE, KERSTIN Inventor name: LEE, MATTHEW Inventor name: KREMOSER, CLAUS Inventor name: KRANZ, HARALD Inventor name: KOGL, MANFRED Inventor name: KOBER, INGO Inventor name: KIELY, JOHN Inventor name: HEBERT, NORMANDC/O PHENEX PHARMACEUTICALS AGGEBAEU Inventor name: HANECAK, RONNIE Inventor name: GIEGRICH, KRISTINA Inventor name: GAHMAN, TIM Inventor name: DNEPROVSKAIA, ELENAC Inventor name: CHERUVALLATH, ZACH Inventor name: BAUER, ULRIKE Inventor name: DEUSCHLE, ULRICH
2013-07-26	STAA	Information on the status of an ep patent application or granted ep patent	Free format text: STATUS: THE APPLICATION IS DEEMED TO BE WITHDRAWN
2013-08-28	18D	Application deemed to be withdrawn	Effective date: 20130301